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Chemical composition of tetraploid Gynostemma pentaphyllum gypenosides and their suppression on inflammatory response by NF‐κB/MAPKs/AP‐1 signaling pathways

机译:四倍体绞股蓝绞股蓝总皂苷的化学成分及其对NF-κB/ MAPKs / AP-1信号通路的炎症反应的抑制

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摘要

The chemical composition and anti‐inflammatory activity of gypenosides isolated from tetraploid (GP) leaves were investigated. The gypenosides accounted for 7.43 mg/g of the tested GP sample, which were composed of four major saponins including isomers of gypenoside 1 and 2 (C H O ), 3 (C H O ), and 4 (C H O ). Pretreatment of gypenosides reduced mRNA expressions of the proinflammatory mediators in LPS‐stimulated RAW264.7 macrophage cells, such as IL‐6, IL‐1β, COX‐2, and TNF‐α in a dose‐dependent manner. The secreted protein levels of IL‐6 and TNF‐α, and NO production were also decreased by gypenosides within the concentration range of 50–200 μg/ml. Moreover, the mechanism studies demonstrated that gypenosides (200 μg/ml) treatment significantly inhibited the nuclear translocation of nuclear factor‐κB and activator protein 1 (c‐Fos and c‐Jun) through down‐regulating the phosphorylation of their upstream IκB kinase and mitogen‐activated protein kinases (MAPKs), especially that of c‐Jun N‐terminal kinase and extracellular regulated protein kinase(JNK and ERK), but not that of the p38 MAPK. These results suggested that the gypenosides might have potential anti‐inflammatory effect and use for improving human health.
机译:研究了从四倍体(GP)叶中分离得到的绞股蓝总皂甙的化学成分和抗炎活性。绞股蓝皂苷占被测GP样品的7.43 mg / g,由四种主要皂苷组成,包括绞股蓝皂苷1和2(C H O),3(C H O)和4(C H O)的异构体。绞股蓝总皂苷的预处理以剂量依赖的方式降低了LPS刺激的RAW264.7巨噬细胞,如IL-6,IL-1β,COX-2和TNF-α中促炎介质的mRNA表达。在50-200μg/ ml的浓度范围内,绞股蓝总皂甙还降低了IL-6和TNF-α的分泌蛋白水平以及NO的产生。此外,机理研究表明,绞股蓝总皂苷(200μg/ ml)处理通过下调其上游IκB激酶和磷酸化的磷酸化来显着抑制核因子κB和激活蛋白1(c-Fos和c-Jun)的核转运丝裂原激活的蛋白激酶(MAPK),尤其是c-Jun N端激酶和细胞外调节蛋白激酶(JNK和ERK)的蛋白,而不是p38 MAPK的蛋白。这些结果表明,绞股蓝总皂甙可能具有潜在的抗炎作用,并可以用于改善人体健康。

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